HZI Community: Abt. Chemische Biologie (CBIO)http://hdl.handle.net/10033/6801
Abt. Chemische Biologie (CBIO)Sun, 02 Aug 2015 20:23:25 GMT2015-08-02T20:23:25ZCytotoxic and antivascular 1-methyl-4-(3-fluoro-4-methoxyphenyl)-5-(halophenyl)-imidazoles.http://hdl.handle.net/10033/364260
Title: Cytotoxic and antivascular 1-methyl-4-(3-fluoro-4-methoxyphenyl)-5-(halophenyl)-imidazoles.
Authors: Biersack, Bernhard; Muthukumar, Yazh; Schobert, Rainer; Sasse, Florenz
Abstract: A series of 1-methyl-4,5-diphenylimidazoles 6 with various patterns of m-halogen substitution at the 5-phenyl ring were tested for cytotoxicity in cancer and nonmalignant cell lines and for their capacity to prevent tube formation in HUVEC cultures. Unlike the monofluoro and difluoro derivatives 6a and 6e, the monobromo and diiodo analogs 6c and 6h were strongly cytotoxic and inhibited the polymerization of tubulin and the tube formation by HUVEC. The dibromo derivative 6g displayed a unique selectivity for KB-3-1 cervix and PC-3 prostate cancer cells. It also inhibited the tube formation by HUVEC and the polymerization of tubulin which is indicative of its potential antiangiogenic activity in solid tumors.Tue, 01 Nov 2011 00:00:00 GMThttp://hdl.handle.net/10033/3642602011-11-01T00:00:00ZPhenotypic plasticity in a willow leaf beetle depends on host plant species: release and recognition of beetle odors.http://hdl.handle.net/10033/346465
Title: Phenotypic plasticity in a willow leaf beetle depends on host plant species: release and recognition of beetle odors.
Authors: Austel, Nadine; Reinecke, Andreas; Björkman, Christer; Hilker, Monika; Meiners, Torsten
Abstract: Aggregation behavior of herbivorous insects is mediated by a wide range of biotic and abiotic factors. It has been suggested that aggregation behavior of the blue willow leaf beetle Phratora vulgatissima is mediated by both host plant odor and by odor released by the beetles. Previous studies show that the beetles respond to plant odors according to their prior host plant experiences. Here, we analyzed the effect of the host plant species on odor released and perceived by adult P. vulgatissima. The major difference between the odor of beetles feeding on salicin-rich and salicin-poor host plants was the presence of salicylaldehyde in the odor of the former, where both males and females released this compound. Electrophysiological studies showed that the intensity of responses to single components of odor released by beetles was sex specific and dependent on the host plant species with which the beetles were fed. Finally, behavioral studies revealed that males feeding on salicin-rich willows were attracted by salicylaldehyde, whereas females did not respond behaviorally to this compound, despite showing clear antennal responses to it. Finally, the ecological relevance of the influence of a host plant species on the plasticity of beetle odor chemistry, perception, and behavior is discussed.Sun, 01 Feb 2015 00:00:00 GMThttp://hdl.handle.net/10033/3464652015-02-01T00:00:00ZAntiviral drug discovery: broad-spectrum drugs from nature.http://hdl.handle.net/10033/344378
Title: Antiviral drug discovery: broad-spectrum drugs from nature.
Authors: Martinez, J P; Sasse, F; Brönstrup, M; Diez, J; Meyerhans, A
Abstract: Covering: up to April 2014. The development of drugs with broad-spectrum antiviral activities is a long pursued goal in drug discovery. It has been shown that blocking co-opted host-factors abrogates the replication of many viruses, yet the development of such host-targeting drugs has been met with scepticism mainly due to toxicity issues and poor translation to in vivo models. With the advent of new and more powerful screening assays and prediction tools, the idea of a drug that can efficiently treat a wide range of viral infections by blocking specific host functions has re-bloomed. Here we critically review the state-of-the-art in broad-spectrum antiviral drug discovery. We discuss putative targets and treatment strategies, with particular focus on natural products as promising starting points for antiviral lead development.Thu, 01 Jan 2015 00:00:00 GMThttp://hdl.handle.net/10033/3443782015-01-01T00:00:00ZInfluence of fenofibrate treatment on triacylglycerides, diacylglycerides and fatty acids in fructose fed rats.http://hdl.handle.net/10033/338621
Title: Influence of fenofibrate treatment on triacylglycerides, diacylglycerides and fatty acids in fructose fed rats.
Authors: Kopf, Thomas; Schaefer, Hans-Ludwig; Troetzmueller, Martin; Koefeler, Harald; Broenstrup, Mark; Konovalova, Tatiana; Schmitz, Gerd
Abstract: Fenofibrate (FF) lowers plasma triglycerides via PPARα activation. Here, we analyzed lipidomic changes upon FF treatment of fructose fed rats. Three groups with 6 animals each were defined as control, fructose-fed and fructose-fed/FF treated. Male Wistar Unilever Rats were subjected to 10% fructose-feeding for 20 days. On day 14, fenofibrate treatment (100 mg/kg p.o.) was initiated and maintained for 7 days. Lipid species in serum were analyzed using mass spectrometry (ESI-MS/MS; LC-FT-MS, GC-MS) on days 0, 14 and 20 in all three groups. In addition, lipid levels in liver and intestine were determined. Short-chain TAGs increased in serum and liver upon fructose-feeding, while almost all TAG-species decreased under FF treatment. Long-chain unsaturated DAG-levels (36:1, 36:2, 36:4, 38:3, 38:4, 38:5) increased upon FF treatment in rat liver and decreased in rat serum. FAs, especially short-chain FAs (12:0, 14:0, 16:0) increased during fructose-challenge. VLDL secretion increased upon fructose-feeding and together with FA-levels decreased to control levels during FF treatment. Fructose challenge of de novo fatty acid synthesis through fatty acid synthase (FAS) may enhance the release of FAs ≤ 16:0 chain length, a process reversed by FF-mediated PPARα-activation.Wed, 01 Jan 2014 00:00:00 GMThttp://hdl.handle.net/10033/3386212014-01-01T00:00:00Z